细胞周期蛋白依赖性激酶9抑制剂研究进展
Research progress in cyclin-dependent kinase 9 inhibitors
曹志豪 1曾扬杰 1李文欣 1张瑞 1王举波 2任晓东1
作者信息
- 1. 贵州大学医学院,贵阳 550025
- 2. 中国药科大学药学院,南京 210009
- 折叠
摘要
细胞周期蛋白依赖性激酶 9(cyclin-dependent kinase 9,CDK9)是CDK家族的一员,属于丝氨酸/苏氨酸蛋白激酶.与其他CDK不同,CDK9 在细胞周期调节中不发挥作用,而是主要参与基因的转录延伸过程.CDK9 能与相应的细胞周期蛋白结合形成正转录延伸因子b(positive transcription elongation factor b,P-TEFb),激活RNA聚合酶Ⅱ并使转录因子磷酸化,从而促进基因转录延伸.研究表明,CDK9 在肿瘤的发病机制中发挥至关重要的作用,使其成为治疗干预的潜在靶标.近年来,CDK9 抑制剂相关研究被广泛报道,部分抑制剂已进入临床试验研究.本文探讨了CDK9 的结构、功能及其与肿瘤的关系,并综述了近年来CDK9 抑制剂研究的最新进展.
Abstract
Cyclin-dependent kinase 9(CDK9)is a member of the CDK family and belongs to the serine/threonine protein kinases.Unlike other CDK,CDK9 does not play a role in cell cycle regulation but is primarily involved in the process of gene transcription elongation.It can form the P-TEFb complex by binding to the corresponding cyclin,activating RNA polymerase Ⅱ,and phosphorylating transcription factors,thereby promoting gene transcription elongation.Research has shown that CDK9 plays a crucial role in the pathogenesis of tumors,making it a potential therapeutic target for intervention.In recent years,the study of CDK9 inhibitors has been widely reported,and some inhibitors have entered clinical trials.This article introduces the structure,function,and relationship of CDK9 with tumors,and reviews the latest development in CDK9 inhibitor research.
关键词
细胞周期蛋白依赖性激酶9/抑制剂/转录/肿瘤/研究进展Key words
cyclin-dependent kinase 9/inhibitor/transcription/tumor/research progress引用本文复制引用
基金项目
贵州省科技计划项目(黔科合基础-ZK[2021]一般556)
贵州大学引进人才科研项目(贵大人基合字202076号)
出版年
2024
NETL
NSTL
万方数据